Patent GB-857194-A (GB)
Title: Therapeutic agents comprising ion-exchange resins
Inventor: TIMMINGTON HERBERT
IPC: A61K31/765
Filed: 1957-07-05
Abstract: Compounds of drugs combined with ionexchange resins are prepared wherein two or more drugs all of which are either acidic or basic in nature are combined with a single quantity of an appropriate (i.e. oppositely charged) cationic or anionic ion-exchange resin which is formed from either a co-polymer of styrene containing acidic or basic groups, or from a polymerized methacrylic acid cross-linked with divinyl benzene and containing carboxylic acid groups.  Specified resins are; strong cationic exchange resins containing sulphonic acid groups, weak cationic exchange resins containing carboxyl groups strong anionic exchange resins containing quaternary ammonium groups, weak anionic exchange resins containing primary amino groups. Examples of "basic" drugs which may be used are; basic alkaloids, e.g. morphine, ephedrine, atropine; basic alkaloids containing acidic groups e.g. trigonelline, arecaidine, ecgonine; antihistamines; basic vitamins e.g. aneurine, pyridoxine, riboflavine; derivatives of phenylalkyl amines.  Examples of "acidic" drugs are; barbituric acid derivatives, aspirin, valerianic acid, acidic vitamins e.g. ascorbic acid, nicotinic acid, pantothenic acid, folic acid.  In specific examples, the preparation is described of; (i) a cross-linked polystyrene resin e.g. Zeokarb 225H or Amberlite IR-120 combined with both hyoscine and hyoscyamine; (ii) a resin of the same type combined with both hyoscyamine and ephedrine; (iii) an anionic exchange resin e.g. De Acidite FF combined with both amylobarbitone and pheno-barbitone.  The compounds are prepared by allowing the resin to react with an aqueous solution of one drug in a soluble form e.g. as an acidic addition or alkali metal salt, until a sufficient amount has combined with the resin and repeating the process with an aqueous solution of the second drug and the resin/drug compound obtained from the first step.  Specification 857,193 is referred to.ALSO:Orally administrable therapeutic preparations comprise two or more drugs all of which are either of basic or acidic nature combined with a single quantity of an appropriate (i.e. oppositely charged) cationic or anionic ion-exchange resin which is formed from either a co-polymer of styrene containing acidic or basic groups, or a polymerised methacrylic acid cross-linked with divinyl benzene and containing carboxylic acid groups.  Specified resins are; (a) strong cationic exchange resins containing the sulphonic acid groups e.g. "Zeokarb" 225, "Amberlite" IR-120, Dowex 50 ("Zeokarb" and "Amberlite" are Registered Trade Marks); (b) weak cationic exchange resins containing the carboxyl group e.g. Zeokarb 226, Amberlite IRC-50; (c) strong anoinic exchange resins containing quaternary ammonium groups e.g. De Acidite FF ("De Acidite" is a Registered Trade Mark), Amberlite IRA-400, Dowex 1 and 2; (d) weak anionic exchange resins containing the primary amino group e.g. DeAcidite E, Amberlite IR-45.  Examples of "basic" drugs which may be used are; basic alkaloides e.g. morphine, ephedrine, atropine; basic alhaloids containing acidic groups e.g. trigonelline, arecaidine, ecgonine; antihistamines; basic vitamins e.g. aneurine, pyridexine, riboflavine; derivatives of phenyl-alkyl amines.  Examples of "acidic" drugs are; barbituric acid derivatives, aspirin, valerianic acid, acidic vitamins e.g. ascorbic acid, nicotinic acid, pantothenic acid, folic acid.  Specific examples of "multiple resin/drug compounds" are hyoscyamine and Hyoseine combined with a sulphuric acid crosslinked polystyrene resin (Zeokarb 225H and Amberlite IR-120); hyoseyamine and ephedrine combined with the same resin type; amylobarbitone and pheno barbitone combined with an anionic exchange resin e.g. De Acidite FF.  The two drugs may be combined with the resin in the desired proportions and, if desired, the combination may be "diluted" by the addition of further pure ion-exchange resin.  The resin/drug compounds may be incorporated into various pharmaceutical forms e.g. tablets, powders, capsules, granules, suspensions in water or oil.  Specification 857,193 is referred to.